Clopidogrel, Prasugrel, Ticagrelor and Ticlopidine are adenosine diphosphate (ADP) receptor antagonists, which can inhibit ADP-mediated platelet activation and aggregation.
Clopidogrel, (S)-alpha-(2-chlorphenyl)-6,7-dihydrothieno [3,2-c]pyridine-5-(4H)acetate hydrogen sulfate, molecular formula C16H16ClNO2SH2SO4, molecular weight 419.9. Common side effects include rash (4%), diarrhea (5%), abdominal pain (6%), dyspepsia (5%), intracranial hemorrhage (0.4%), digestive tract hemorrhage (2%), serious granulocyte reduction (0.04%). Results are mainly from a large clinical trial (CAPRIE). The general tolerance of clopidogrel in the study is equivalent to that of ASA, and is unrelated to age, race and gender. Hemorrhagic diseases include gastrointestinal hemorrhage, purpura, congestion, hematoma, epistaxis, hematuria, ocular hemorrhage (mainly conjunctival hemorrhage) and intracranial hemorrhage. The severe bleeding rate of Clopidogrel-treated patients is 1.4%. In blood system, it includes severe neutrophile granulocyte reduction, aplastic anemia and serious platelet reduction, which are relatively rare.
Prasugrel, 2-[2-(acetoxyl)-6,7-dihydrothieno [3,2-c]pyridine-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl))ethanone, molecular formula: C20H20FNO3S, molecular weight: 373.44. Clinically, it is used to treat cardiovascular and cerebrovascular diseases such as heart failure, stroke, unstable angina. To patients with acute coronary syndrome and requiring percutaneous coronary intervention surgery, the effect of Prasugrel is better than that of Clopidogrel, but the carcinogenesis risk is high, and the hemorrhage risk of prasurel is also higher than that of Clopidogrel.
Ticagrelor, molecular formula: C23H28F2N6O4S, molecular weight: 522.57, (1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3,4-Difluorophenyl)cycloprolamino]-5-(propyl sulfanyl)-3H-[1,2,3]triazolo [4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy) cyclopenane-1,2-diol. In patients treated with Ticagrelor, the most frequently reported side effects are dyspnea, contusion and nasal hemorrhage, and the occurrence rate of Ticagrelor is higher than that of the Clopidogrel. Other common side effects include gastrointestinal hemorrhage, subcutaneous or dermis bleeding, blood stasis and operation site bleeding. Occasional side effects include intracranial hemorrhage, dizziness and headache, eye hemorrhage, hemoptysis, hematemesis, gastrointestinal ulcer hemorrhage, hemorrhoids bleeding, gastritis, oral bleeding, emesis, diarrhea, abdominal pain, nausea, dyspepsia, itching, rash, urethra and vagina bleeding, and postoperative bleeding. Rare side effects include: hyperuricemia, consciousness disorder, sensory abnormality, ear hemorrhage, dizziness and dizziness, post-peritoneal bleeding, constipation, hemarthrosis, blood creatinine rise, wound bleeding, traumatic bleeding, wound bleeding, wound bleeding, blood creatinine rise, wound bleeding, traumatic bleeding. In the PLATO study, the occurrence rate of interventricular interval among Ticagrelor-treated patients in the acute stage is 60%; the occurrence rate of the interventricular interval after one month is 2.2%.
Ticlopidine, molecular formula: C14H14ClNS; molecular weight: 263.79. It is mainly used for chronic thromboangiitis obliterans, obliterative arteriosclerosis, myocardial infarction, cerebral ischemia and so on. It has an inhibitory effect on platelet aggregation induced by collagen, thrombin, arachidonic acid, epinephrine, and platelet activation factor and the like. Moreover, it has a certain depolymerization effect. Common side effects include digestive tract symptoms (such as nausea, abdominal discomfort and diarrhea) and rash. The occurrence rate is about 10% and can be reduced by a postprandial administration. Common side effects also include hemorrhage and gastrointestinal disease such as nausea, emesis and diarrhea, which can be alleviated by a postprandial administration. Allergic reactions, such as urticaria and rash, mainly occur in the first month of treatment. Hematological changes such as leukopenia, granulocyte deficiency, whole blood cell reduction, erythroleukemia. If any early sign is found, the medicine should be immediately stopped. Cholestasis jaundice and the like can also be found occasionally.
Therefore, how to reduce the side effect through reducing the use of Clopidogrel, Prasugrel, Ticagrelor and Ticlopidine without losing the treatment effect requires a solution.
Ginkgolide B is the most potent antagonist against platelet activation factor that has been found heretofore. It has been used to treat phlegm and blood stasis obstruction of ischemic stroke. However, its price is high and clinical usage cost is high.